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Compound Detail

CHEMBL430084

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CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(N)=O)C1c1ccc(OC)cc1

Basic Information

ChEMBL ID CHEMBL430084
Phase Preclinical
Structure Type MOL
InChI Key QFVSJYNKQYXIFC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

509.6
MW (Da)
4.09
ALogP
6
HBA
1
HBD
94.3
PSA (Ų)
0.46
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39N3O5
MW 509.65
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -0.43

Activity Summary

IC50 1 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4566
IC50 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 58.0 nM 7.24 Inhibitory activity against the Endothelin A receptor of rat MMQ cells 8676339

Literature References

PubMed DOI Target Context # Activities
8676339 10.1021/jm9505369 Endothelin-1 receptor 1
8676339 10.1021/jm9505369 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine